PE20090418A1 - POLICYCLIC GUANINE DERIVATIVES AND THEIR METHODS OF USE - Google Patents
POLICYCLIC GUANINE DERIVATIVES AND THEIR METHODS OF USEInfo
- Publication number
- PE20090418A1 PE20090418A1 PE2008001040A PE2008001040A PE20090418A1 PE 20090418 A1 PE20090418 A1 PE 20090418A1 PE 2008001040 A PE2008001040 A PE 2008001040A PE 2008001040 A PE2008001040 A PE 2008001040A PE 20090418 A1 PE20090418 A1 PE 20090418A1
- Authority
- PE
- Peru
- Prior art keywords
- aryl
- alkyl
- compounds
- alkylen
- optionally
- Prior art date
Links
- UYTPUPDQBNUYGX-UHFFFAOYSA-N guanine Chemical class O=C1NC(N)=NC2=C1N=CN2 UYTPUPDQBNUYGX-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- WJSVJNDMOQTICG-UHFFFAOYSA-N 2-amino-1-[(2-methyl-4-methylidene-5-oxooxolan-2-yl)methyl]-7h-purin-6-one Chemical class NC1=NC=2N=CNC=2C(=O)N1CC1(C)CC(=C)C(=O)O1 WJSVJNDMOQTICG-UHFFFAOYSA-N 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 208000000094 Chronic Pain Diseases 0.000 abstract 1
- 102100037602 P2X purinoceptor 7 Human genes 0.000 abstract 1
- 101710189965 P2X purinoceptor 7 Proteins 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 230000009977 dual effect Effects 0.000 abstract 1
- 210000002865 immune cell Anatomy 0.000 abstract 1
- 208000004296 neuralgia Diseases 0.000 abstract 1
- 208000021722 neuropathic pain Diseases 0.000 abstract 1
- 201000008482 osteoarthritis Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/14—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE GUANINA POLICICLICOS DE FORMULA (I) DONDE R1 ES ALQUILO(C1-C6) O ALQUILO(C1-C6)-ALQUILEN-O; R2 ES ALQUILO(C1-C20), ARILO(C6-C14), -ALQUILEN-ARILO, ENTRE OTROS, OPCIONALMENTE SUSTITUIDOS CON R5, DONDE R5 ES DE 1 A 3 GRUPOS DE ALQUENILO(C2-C15), ALQUINILO(C2-C15), ARILO(C6-C14), HALO, ENTRE OTROS; R3 ES ALQUILO(C1-C20), ALQUILEN-ARILO, CICLOALQUILO(C3-C10), ALQUILENO-HETEROCICLOALQUILO, ENTRE OTROS, DONDE ARILO, CICLOALQUILO O HETEROCICLOALQUILO ESTAN OPCIONALMENTE SUSTITUIDOS CON R7, EN DONDE R7 ES DE 1 A 3 GRUPOS DE ALQUILO(C1-C6), HALO, ARILO(C6-C14), ENTRE OTROS; R4 ES H, ALQUILO(C1-C6), ENTRE OTROS. SON COMPUESTOS PREFERIDOS LOS COMPUESTOS DE FORMULA (i), (ii), ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON ANTAGONISTAS DEL CANAL IONICO P2X7 DE LAS CELULAS INMUNES SIENDO UTILES EN EL TRATAMIENTO DE ARTRITIS REUMATOIDE, OSTEOARTRITIS, ASMA, ENFERMEDAD PULMONAR OBSTRUCTIVA CRONICA, DOLOR NEUROPATICO, DOLOR CRONICOREFERS TO POLYCYCLIC GUANINE DERIVATIVE COMPOUNDS OF FORMULA (I) WHERE R1 IS ALKYL (C1-C6) OR ALKYL (C1-C6) -ALKYLEN-O; R2 IS ALKYL (C1-C20), ARYL (C6-C14), -ALKYLEN-ARYL, AMONG OTHERS, OPTIONALLY SUBSTITUTED WITH R5, WHERE R5 IS FROM 1 TO 3 ALKENYL GROUPS (C2-C15), ALKYLEN (C2-C15 ), ARYL (C6-C14), HALO, AMONG OTHERS; R3 IS ALKYL (C1-C20), ALKYL-ARYL, CYCLOALKYL (C3-C10), ALKYLENE-HETEROCYCLOALKYL, AMONG OTHERS, WHERE ARYL, CYCLOALKYL OR HETEROCYLALKYL, OPTIONALLY 1 ROLLS OF 3 RYLS OF AYL7, WITH OPTIONALLY 3 ROLLS OF DUAL AYL7. (C1-C6), HALO, ARYL (C6-C14), AMONG OTHERS; R4 IS H, ALKYL (C1-C6), AMONG OTHERS. PREFERRED COMPOUNDS ARE THE COMPOUNDS OF FORMULA (i), (ii), AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SAID COMPOUNDS ARE ANTAGONISTS OF THE P2X7 ION CHANNEL OF IMMUNE CELLS, BEING USEFUL IN THE TREATMENT OF RHEUMATOID ARTHRITIS, OSTEOARTHRITIS, ASTHMA, CHRONIC OBSTRUCTIVE PULMONARY DISEASE, NEUROPATHIC PAIN, CHRONIC PAIN
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94545207P | 2007-06-21 | 2007-06-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20090418A1 true PE20090418A1 (en) | 2009-04-18 |
Family
ID=40186205
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008001040A PE20090418A1 (en) | 2007-06-21 | 2008-06-18 | POLICYCLIC GUANINE DERIVATIVES AND THEIR METHODS OF USE |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8349858B2 (en) |
| EP (1) | EP2170896A2 (en) |
| JP (1) | JP2010530427A (en) |
| KR (1) | KR20100023040A (en) |
| AR (1) | AR067060A1 (en) |
| AU (1) | AU2008269177A1 (en) |
| BR (1) | BRPI0812909A2 (en) |
| CA (1) | CA2691194A1 (en) |
| CL (1) | CL2008001835A1 (en) |
| CO (1) | CO6251257A2 (en) |
| EC (1) | ECSP099822A (en) |
| IL (1) | IL202754A0 (en) |
| MX (1) | MX2010000098A (en) |
| PE (1) | PE20090418A1 (en) |
| RU (1) | RU2010101611A (en) |
| TW (1) | TW200911817A (en) |
| WO (1) | WO2009002423A2 (en) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2523561A4 (en) * | 2009-12-22 | 2013-06-05 | Merck Sharp & Dohme | 7,8-DIHYDRO-1H-IMIDAZO [2,1-B] PURIN-4 (5H) -ONE DERIVATIVES AND METHODS OF USE THEREOF |
| WO2012078448A1 (en) * | 2010-12-06 | 2012-06-14 | Schering Corporation | Tricyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors |
| TWI589576B (en) * | 2011-07-15 | 2017-07-01 | 諾華公司 | Salts of aza-bicyclic diaryl ethers and methods of making same or their precursors |
| MX341834B (en) * | 2011-12-30 | 2016-09-05 | Dow Agrosciences Llc | Methods of forming 4-chloro-2-fluoro-3-substituted-phenylboronic acid pinacol esters and methods of using the same. |
| DK2948148T3 (en) | 2013-01-28 | 2020-10-26 | Incozen Therapeutics Pvt Ltd | METHODS FOR TREATMENT OF AUTOIMMUNE, RESPIRATORY AND INFLAMMATORY DISORDERS BY INHALATION OF ROFLUMILAST N-OXIDE |
| WO2014152589A1 (en) | 2013-03-14 | 2014-09-25 | Janssen Pharmaceutica Nv | P2x7 modulators |
| WO2014152537A1 (en) * | 2013-03-14 | 2014-09-25 | Janssen Pharmaceutica Nv | P2x7 modulators |
| TWI599567B (en) | 2013-03-14 | 2017-09-21 | 健生藥品公司 | P2X7 regulator |
| JO3509B1 (en) | 2013-03-14 | 2020-07-05 | Janssen Pharmaceutica Nv | P2x7 modulators |
| EP3191488B1 (en) | 2014-09-12 | 2019-08-14 | Janssen Pharmaceutica NV | P2x7 modulating n-acyl-triazolopyrazines |
| JP6592510B2 (en) | 2014-09-12 | 2019-10-16 | ヤンセン ファーマシューティカ エヌ.ベー. | P2X7 regulator |
| TWI715569B (en) | 2015-04-24 | 2021-01-11 | 日商塩野義製藥股份有限公司 | Six-membered heterocyclic derivatives and pharmaceutical composition comprising the same |
| US11066409B2 (en) | 2016-10-17 | 2021-07-20 | Shionogi & Co., Ltd. | Bicyclic nitrogen-containing heterocyclic derivatives and pharmaceutical composition comprising the same |
| WO2020065614A1 (en) | 2018-09-28 | 2020-04-02 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
| CR20210153A (en) | 2018-09-28 | 2021-05-11 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
| CA3156100A1 (en) | 2019-09-30 | 2021-04-08 | Janssen Pharmaceutica Nv | MGL PET RADIOLABE LIGANDS |
| US11891387B2 (en) | 2020-03-26 | 2024-02-06 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0119372A1 (en) | 1983-03-21 | 1984-09-26 | Svecia Silkscreen Maskiner AB | Conveying device using a number of rollers |
| IL98559A0 (en) | 1990-06-21 | 1992-07-15 | Schering Corp | Polycyclic guanine derivatives |
| AU681875B2 (en) * | 1993-02-26 | 1997-09-11 | Schering Corporation | 2-benzyl-polycyclic guanine derivatives and process for preparing them |
| JPH10501122A (en) | 1994-05-27 | 1998-02-03 | グラクソ、グループ、リミテッド | P ▲ 2X ▼ receptor (purinoceptor family) |
| US5856129A (en) | 1996-10-30 | 1999-01-05 | Incyte Pharmaceuticals, Inc. | DNA encoding a human purinoceptor |
| WO1999055901A2 (en) | 1998-04-30 | 1999-11-04 | Abbott Laboratories | Screening assay for identifying human purinoreceptor ligands |
| AU1535002A (en) | 2000-10-13 | 2002-04-22 | Bristol Myers Squibb Co | Methods for detecting modulators of ion channels using thallium (i) sensitive assays |
| US20020182646A1 (en) | 2001-04-30 | 2002-12-05 | Ke Huazhu | Methods and products for identifying modulators of P2X7 receptor activity, and their use in the treatment of skeletal disorders |
| CA2457944C (en) * | 2001-08-28 | 2009-09-29 | Schering Corporation | Polycyclic guanine phosphodiesterase v inhibitors |
| US20050123925A1 (en) | 2002-11-15 | 2005-06-09 | Genentech, Inc. | Compositions and methods for the diagnosis and treatment of tumor |
| US20050238650A1 (en) | 2002-04-17 | 2005-10-27 | Genentech, Inc. | Compositions and methods for the treatment of tumor of hematopoietic origin |
| WO2003042216A1 (en) * | 2001-11-09 | 2003-05-22 | Schering Corporation | Polycyclic guanine derivative phosphodiesterase v inhibitors |
| US7560243B2 (en) | 2003-04-21 | 2009-07-14 | Wisconsin Alumni Research Foundation | White blood cell functional assay |
| GB0323147D0 (en) | 2003-10-03 | 2003-11-05 | Medical Res Council | Improvements in or relating to concentration of intracellular agents |
| CA2608504A1 (en) | 2005-05-31 | 2006-12-07 | Duska Scientific Co. | Inhibition of neuronal damage |
| WO2007115192A2 (en) | 2006-03-31 | 2007-10-11 | Abbott Laboratories | P2x7 antagonists to treat affective disorders |
-
2008
- 2008-06-18 JP JP2010513236A patent/JP2010530427A/en not_active Withdrawn
- 2008-06-18 EP EP08768585A patent/EP2170896A2/en not_active Withdrawn
- 2008-06-18 MX MX2010000098A patent/MX2010000098A/en not_active Application Discontinuation
- 2008-06-18 US US12/663,727 patent/US8349858B2/en not_active Expired - Fee Related
- 2008-06-18 AU AU2008269177A patent/AU2008269177A1/en not_active Abandoned
- 2008-06-18 CA CA2691194A patent/CA2691194A1/en not_active Abandoned
- 2008-06-18 BR BRPI0812909-6A2A patent/BRPI0812909A2/en not_active Application Discontinuation
- 2008-06-18 PE PE2008001040A patent/PE20090418A1/en not_active Application Discontinuation
- 2008-06-18 KR KR1020107001339A patent/KR20100023040A/en not_active Withdrawn
- 2008-06-18 WO PCT/US2008/007592 patent/WO2009002423A2/en not_active Ceased
- 2008-06-18 RU RU2010101611/04A patent/RU2010101611A/en not_active Application Discontinuation
- 2008-06-19 AR ARP080102611A patent/AR067060A1/en not_active Application Discontinuation
- 2008-06-19 TW TW097122895A patent/TW200911817A/en unknown
- 2008-06-19 CL CL2008001835A patent/CL2008001835A1/en unknown
-
2009
- 2009-12-15 IL IL202754A patent/IL202754A0/en unknown
- 2009-12-17 CO CO09144826A patent/CO6251257A2/en not_active Application Discontinuation
- 2009-12-21 EC EC2009009822A patent/ECSP099822A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL202754A0 (en) | 2010-06-30 |
| EP2170896A2 (en) | 2010-04-07 |
| AU2008269177A1 (en) | 2008-12-31 |
| ECSP099822A (en) | 2010-01-29 |
| US20110065738A1 (en) | 2011-03-17 |
| WO2009002423A3 (en) | 2009-04-23 |
| BRPI0812909A2 (en) | 2014-12-09 |
| RU2010101611A (en) | 2011-07-27 |
| TW200911817A (en) | 2009-03-16 |
| JP2010530427A (en) | 2010-09-09 |
| CL2008001835A1 (en) | 2008-12-26 |
| KR20100023040A (en) | 2010-03-03 |
| MX2010000098A (en) | 2010-04-21 |
| WO2009002423A2 (en) | 2008-12-31 |
| CO6251257A2 (en) | 2011-02-21 |
| US8349858B2 (en) | 2013-01-08 |
| CA2691194A1 (en) | 2008-12-31 |
| AR067060A1 (en) | 2009-09-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |